Traceless solid-phase synthesis of N1,N7-disubstituted purines

被引:16
|
作者
Fu, H [1 ]
Lam, YL [1 ]
机构
[1] Natl Univ Singapore, Dept Chem, Singapore 117543, Singapore
来源
JOURNAL OF COMBINATORIAL CHEMISTRY | 2005年 / 7卷 / 05期
关键词
D O I
10.1021/cc050058f
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
A highly regioselective and traceless solid-phase route to N1,N7-disubstituted purines has been developed. Key steps in the reaction strategy involves (i) coupling of 6-chloropurine to the REM resin (Michael addition), (ii) oxidation, (iii) N1-alkylation, (iv) quaternization, and (v) product release through Hofmann elimination. A library of 15 N1,N7-disubstituted purines was synthesized.
引用
收藏
页码:734 / 738
页数:5
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